Product Name :
CC-930
Description:
CC-930, also known as Tanzisertib, is a potent, selective, and orally active JNK inhibitor with potential antifibrotic activity. CC-930 entered Phase I clinical trials. Tanzisertib may have potential use for prevention and treatment of dermal fibrosis. Selective inhibition of JNK by CC-930 exerted potent antifibrotic effects in vitro and in different models in vivo. JNK might thus be a novel molecular target for the treatment of fibrosis in SSc.
CAS:
899805-25-5
Molecular Weight:
448.44
Formula:
C21H23F3N6O2
Chemical Name:
(1S,4r)-4-((9-((S)-tetrahydrofuran-3-yl)-8-((2,4,6-trifluorophenyl)amino)-9H-purin-2-yl)amino)cyclohexanol JNK-930; JNKI-1
Smiles :
OC1CCC(CC1)NC1=NC2=C(C=N1)N=C(NC1C(F)=CC(F)=CC=1F)N2[C@@H]1COCC1
InChiKey:
IBGLGMOPHJQDJB-MOKVOYLWSA-N
InChi :
InChI=1S/C21H23F3N6O2/c22-11-7-15(23)18(16(24)8-11)28-21-27-17-9-25-20(26-12-1-3-14(31)4-2-12)29-19(17)30(21)13-5-6-32-10-13/h7-9,12-14,31H,1-6,10H2,(H,27,28)(H,25,26,29)/t12?,13-,14?/m0/s1
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
CC-930, also known as Tanzisertib, is a potent, selective, and orally active JNK inhibitor with potential antifibrotic activity. CC-930 entered Phase I clinical trials. Tanzisertib may have potential use for prevention and treatment of dermal fibrosis. Selective inhibition of JNK by CC-930 exerted potent antifibrotic effects in vitro and in different models in vivo. JNK might thus be a novel molecular target for the treatment of fibrosis in SSc.{{Imipramine} medchemexpress|{Imipramine} Autophagy|{Imipramine} Protocol|{Imipramine} In Vitro|{Imipramine} manufacturer|{Imipramine} Cancer} |Product information|CAS Number: 899805-25-5|Molecular Weight: 448.44|Formula: C21H23F3N6O2|Synonym:|Tanzisertib|CC 930|JNK-930|JNKI1|JNKI 1|CC930|CC-930|JNKI-1|JNK930|JNK 930|Chemical Name: (1S,4r)-4-((9-((S)-tetrahydrofuran-3-yl)-8-((2,4,6-trifluorophenyl)amino)-9H-purin-2-yl)amino)cyclohexanol JNK-930; JNKI-1|Smiles: OC1CCC(CC1)NC1=NC2=C(C=N1)N=C(NC1C(F)=CC(F)=CC=1F)N2[C@@H]1COCC1|InChiKey: IBGLGMOPHJQDJB-MOKVOYLWSA-N|InChi: InChI=1S/C21H23F3N6O2/c22-11-7-15(23)18(16(24)8-11)28-21-27-17-9-25-20(26-12-1-3-14(31)4-2-12)29-19(17)30(21)13-5-6-32-10-13/h7-9,12-14,31H,1-6,10H2,(H,27,28)(H,25,26,29)/t12?,13-,14?/m0/s1|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO: 89 mg/mLwarmed(183.54 mM). Water: 4 mg/mLwarmed(8.24 mM).|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined.|HS Tariff Code: 382200|How to use|In Vitro:|CC-930 inhibits the formation of phospho-cJun in human PBMC stimulated by phorbol-12-myristate-13-acetate and phytohemeagglutinin (IC50=1 μM). CC-930 (1-2 μM) substantially reduces hepatocyte apoptosis and necrosis, abrogates apoptosis and necrosis in FC-loaded WT hepatocytes. CC-930 blocks the JNK pathway that is activated by pro-fibrotic cytokines in systemic sclerosis.|In Vivo:|CC-930 (10 and 30 mg/kg, p.o.) inhibits the production of TNFa by 23% and 77% in the acute rat LPS-induced TNFa production PK-PD model.{{Deruxtecan} MedChemExpress|{Deruxtecan} Drug-Linker Conjugates for ADC|{Deruxtecan} Technical Information|{Deruxtecan} In Vivo|{Deruxtecan} supplier|{Deruxtecan} Autophagy} CC-930 (150 mg/kg) prevents the development of fibrosis in different models, but can also induce the regression of pre-existing fibrosis.PMID:23357584 |References:|Gan LT, Van Rooyen DM, Koina M, McCuskey RS, Teoh NC, Farrell GC. Hepatocyte free cholesterol lipotoxicity results from JNK1-mediated mitochondrial injury and is HMGB1 and TLR4-dependent. J Hepatol. 2014 Jul 23. pii: S0168-8278(14)00523-6. doi: 10.1016/j.jhep.2014.07.024. [Epub ahead of print] PubMed PMID: 25064435.Atsriku C, Hoffmann M, Ye Y, Kumar G, Surapaneni S. Metabolism and disposition of a potent and selective JNK inhibitor [14C]tanzisertib following oral administration to rats, dogs and humans. Xenobiotica. 2015 May;45(5):428-41. doi: 10.3109/00498254.2014.990949. PubMed PMID: 25482583.Atsriku C, Hoffmann M, Moghaddam M, Kumar G, Surapaneni S. In vitro metabolism of a novel JNK inhibitor tanzisertib: interspecies differences in oxido-reduction and characterization of enzymes involved in metabolism. Xenobiotica. 2015;45(6):465-80. doi: 10.3109/00498254.2014.991367. PubMed PMID: 25475995.Products are for research use only. Not for human use.|